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GABA receptor alpha-5 subunit Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
Ethyl 8-chloro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo(1,5-a)(1,4)benzodiazepine-3-carboxylateKi0.85 [1], 54.6 [2]
8-Methyl-5-[4-(trifluoromethyl)-1-benzothiophen-2-yl]-1,9-dihydro-[1,3]oxazolo[4,5-h][2,3]benzodiazepin-2-oneIC50201.0 [1], 500.0 [2]
SaripidemIC502.7 [1], 4.6 [2]
ZolpidemKi15000.0 [1]
Ethyl-8-azido-5,6-dihydro-5-methyl-6-oxo-4H-imidazo-1,4-benzodiazepine-3-carboxylateKi3.1 [1]
EszopicloneKi15000.0 [1]
Ethyl (7S)-15-methoxy-12-oxo-2,4,11-triazatetracyclo[11.4.0.02,6.07,11]heptadeca-1(17),3,5,13,15-pentaene-5-carboxylateKi0.45 [1]
L-838417Ki2.3 [1]
3-[3-Tert-butyl-2-[(2-methyl-1,2,4-triazol-3-yl)methoxy]pyrazolo[1,5-d][1,2,4]triazin-7-yl]-5-methyl-1,2-oxazoleKi1.4 [1]
1-Methyl-5-phenyl-1,3-dihydro-benzo[e][1,4]diazepin-2-oneIC5010000.0 [1]
Unii-ZD6M94A8IHIC50200.0 [1]
N-(2-Oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-acetamideIC5010000.0 [1]
BasmisanilKi4.7 [1]
13-(4-Methyl-1,3-thiazol-2-yl)-15-pyridin-4-yl-4,11-diazatricyclo[9.4.0.02,7]pentadeca-1(15),2(7),3,5,13-pentaen-12-oneKi33.3 [1]
4-Bromo-3,5-dimethyl-1-((4-(3-nitrophenyl)thiazol-2-yl)methyl)-1H-pyrazoleIC5010000.0 [1]
N-(4-Chlorophenyl)-5-(2-(methylthio)pyrimidin-4-yl)thiophene-2-sulfonamideIC5010000.0 [1]
1-(4-Chlorobenzoyl)-6,6-dimethyl-3-methylsulfanyl-1,3,3a,5,7,7a-hexahydro-2-benzothiophen-4-oneIC50210.0 [1]
1-(4-Chlorobenzoyl)-3-(methylthio)-hexahydrobenzo[c]thiophen-4(1H)-oneIC50550.0 [1]
6,6-Dimethyl-3-methylsulfanyl-1-(3-nitrobenzoyl)-1,3,3a,5,7,7a-hexahydro-2-benzothiophen-4-oneIC5010000.0 [1]
(3-Aminobenzo[b]thiophen-2-yl)(4-chlorophenyl)methanoneIC501000.0 [1]
7-Chloro-3-(ethoxymethyl)-4-methylimidazo[1,5-a]quinazolin-5-oneKi83.0 [1]
7-Chloro-3-(chloromethyl)-4-methylimidazo[1,5-a]quinazolin-5-oneKi500.0 [1]
Tert-butyl 7-chloro-4-methyl-5-oxoimidazo[1,5-a]quinazoline-3-carboxylateKi0.65 [1]
Cyclopropylmethyl 7-chloro-4-methyl-5-oxoimidazo[1,5-a]quinazoline-3-carboxylateKi9.8 [1]
3-Acetyl-7-chloro-4-methylimidazo[1,5-a]quinazolin-5(4H)-oneKi2610.0 [1]
7-Chloro-4-methyl-3-pentanoylimidazo[1,5-a]quinazolin-5(4H)-oneKi166.0 [1]
7-Chloro-3-(hydroxymethyl)-4-methylimidazo[1,5-a]quinazolin-5(4H)-oneKi300.0 [1]
7-Chloro-3-ethyl-4-methylimidazo[1,5-a]quinazolin-5(4H)-oneKi182.0 [1]
7-Chloro-4-methyl-3-pentylimidazo[1,5-a]quinazolin-5(4H)-oneKi369.0 [1]
15-Methoxy-12-oxa-9-aza-3-azoniatetracyclo[9.7.0.03,8.013,18]octadeca-1(11),3,5,7,13(18),14,16-heptaen-10-one;chlorideKi2364.0 [1]
3-Iodo-5-oxido-N-(pyridin-3-ylmethyl)pyrazolo[5,1-c][1,2,4]benzotriazin-5-ium-8-amineKi24.9 [1]
5-(6-Fluoro-1-benzothiophen-2-yl)-8-methyl-1,9-dihydro-[1,3]oxazolo[4,5-h][2,3]benzodiazepin-2-oneIC50100.0 [1]
5-[3-Chloro-4-(trifluoromethyl)-1-benzothiophen-2-yl]-8-methyl-1,9-dihydro-[1,3]oxazolo[4,5-h][2,3]benzodiazepin-2-oneIC50250.0 [1]
5-(1-Benzothiophen-2-yl)-8-methyl-1,9-dihydro-[1,3]oxazolo[4,5-h][2,3]benzodiazepin-2-oneIC50130.0 [1]
6-[(5-Methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]-N-propan-2-ylpyridine-3-carboxamideKi1.3 [1]
N-Cyclopropyl-6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]pyridine-3-carboxamideKi2.7 [1]
N-Cyclobutyl-6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]pyridine-3-carboxamideKi2.8 [1]
N-Cyclopentyl-6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]pyridine-3-carboxamideKi3.9 [1]
6-[(5-Methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]-N-(1-propan-2-ylpiperidin-4-yl)pyridine-3-carboxamideKi9.9 [1]
N-(1-Benzylpiperidin-4-yl)-6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]pyridine-3-carboxamideKi7.3 [1]
N-(1-Ethylpiperidin-3-yl)-6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]pyridine-3-carboxamideKi5.0 [1]
4-Benzyloxy-2-(5-methyl-3-phenyl-isoxazol-4-ylmethoxy)-pyridineKi35.1 [1]
2-[(5-Methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]-N-(2,2,2-trifluoroethyl)pyridine-4-carboxamideKi37.8 [1]
6-[(5-Methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]-N-(oxan-4-yl)-4-(trifluoromethyl)pyridine-3-carboxamideKi10.7 [1]
5-Methyl-6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]-N-(oxan-4-yl)pyridine-3-carboxamideKi1.4 [1]
6-[[3-(2-Fluorophenyl)-5-methyl-1,2-oxazol-4-yl]methoxy]-N-(2,2,3,3,3-pentafluoropropyl)pyridine-3-carboxamideKi9.8 [1]
6-[[3-(2-Fluorophenyl)-5-methyl-1,2-oxazol-4-yl]methoxy]-N-propan-2-ylpyridine-3-carboxamideKi3.6 [1]
6-[[3-(3-Fluorophenyl)-5-methyl-1,2-oxazol-4-yl]methoxy]-N-(2,2,2-trifluoroethyl)pyridine-3-carboxamideKi3.0 [1]
6-[[3-(3-Chlorophenyl)-5-methyl-1,2-oxazol-4-yl]methoxy]-N-(cyclopropylmethyl)pyridine-3-carboxamideKi8.1 [1]
6-[[3-(3-Chlorophenyl)-5-methyl-1,2-oxazol-4-yl]methoxy]-N-cyclopropylpyridine-3-carboxamideKi7.6 [1]
6-[[3-(4-Fluorophenyl)-5-methyl-1,2-oxazol-4-yl]methoxy]-N-(2,2,2-trifluoroethyl)pyridine-3-carboxamideKi1.2 [1]
N-(Cyclopropylmethyl)-6-[[3-(4-fluorophenyl)-5-methyl-1,2-oxazol-4-yl]methoxy]pyridine-3-carboxamideKi1.5 [1]
6-[[3-(4-Fluorophenyl)-5-methyl-1,2-oxazol-4-yl]methoxy]-N-propan-2-ylpyridine-3-carboxamideKi0.7 [1]
6-[3-(4-Chloro-phenyl)-5-methyl-isoxazol-4-ylmethoxy]-nicotinic acid methyl esterKi4.5 [1]
6-[[3-(4-Chlorophenyl)-5-methyl-1,2-oxazol-4-yl]methoxy]-N-(2,2,2-trifluoroethyl)pyridine-3-carboxamideKi2.1 [1]
6-[[3-(4-Fluorophenyl)-5-(trifluoromethyl)-1,2-oxazol-4-yl]methoxy]-N-(oxan-4-yl)pyridine-3-carboxamideKi12.5 [1]
N-Cyclopropyl-6-[(5-methyl-3-pyridin-4-yl-1,2-oxazol-4-yl)methoxy]pyridine-3-carboxamideKi7.1 [1]
6-[(5-Methyl-3-pyridin-4-yl-1,2-oxazol-4-yl)methoxy]-N-(2,2,2-trifluoroethyl)pyridine-3-carboxamideKi5.9 [1]
N-(Cyclopropylmethyl)-6-[(5-methyl-3-pyridin-4-yl-1,2-oxazol-4-yl)methoxy]pyridine-3-carboxamideKi4.1 [1]
N-Cyclopropyl-6-[[3-(4-fluorophenyl)-5-methyl-1,2-oxazol-4-yl]methylamino]pyridine-3-carboxamideKi7.4 [1]
6-[[3-(4-Fluorophenyl)-5-methyl-1,2-oxazol-4-yl]methylamino]-N-(oxan-4-yl)pyridine-3-carboxamideKi6.5 [1]
N-(1-Hydroxy-2-methylpropan-2-yl)-6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]pyridine-3-carboxamideKi10.0 [1]
N-(2-Methoxyethyl)-6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]pyridine-3-carboxamideKi7.8 [1]
N-(1-Hydroxypropan-2-yl)-6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]pyridine-3-carboxamideKi1.0 [1]
N-(2-Hydroxycyclohexyl)-6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]pyridine-3-carboxamideKi2.9 [1]
N-(2-Hydroxy-2-methylpropyl)-6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]pyridine-3-carboxamideKi2.3 [1]
N-[(1R,2R)-2-Hydroxycyclohexyl]-6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]pyridine-3-carboxamideKi11.0 [1]
N-[(1R,2S)-2-Hydroxycyclohexyl]-6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]pyridine-3-carboxamideKi4.8 [1]
N-[(1S,2R)-2-Hydroxycyclohexyl]-6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]pyridine-3-carboxamideKi4.4 [1]
N-[(1S,2S)-2-Hydroxycyclohexyl]-6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]pyridine-3-carboxamideKi6.5 [1]
N-(2-Hydroxycyclopentyl)-6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]pyridine-3-carboxamideKi3.9 [1]
N-(1,3-Dihydroxypropan-2-yl)-6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]pyridine-3-carboxamideKi1.7 [1]
N-[(2S)-1-Hydroxybutan-2-yl]-6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]pyridine-3-carboxamideKi0.7 [1]
N-[(2R)-1-Hydroxybutan-2-yl]-6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]pyridine-3-carboxamideKi2.3 [1]
N-[(1R,2S)-2-Hydroxycyclopentyl]-6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]pyridine-3-carboxamideKi5.0 [1]
N-[(1S,2R)-2-Hydroxycyclopentyl]-6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]pyridine-3-carboxamideKi2.7 [1]
6-[(5-Methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]-N-[2-(2-oxoimidazolidin-1-yl)ethyl]pyridine-3-carboxamideKi4.3 [1]
N-(3-Hydroxybutyl)-6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]pyridine-3-carboxamideKi2.3 [1]
Tert-butyl N-[2-[[6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]pyridine-3-carbonyl]amino]ethyl]carbamateKi8.4 [1]
Tert-butyl 3-[[6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]pyridine-3-carbonyl]amino]azetidine-1-carboxylateKi4.5 [1]
6-[(5-Methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]-N-[(2S)-1,1,1-trifluoropropan-2-yl]pyridine-3-carboxamideKi1.9 [1]
6-[(5-Methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]-N-(1-methylpyrazol-4-yl)pyridine-3-carboxamideKi1.1 [1]
N-Cyclopropylsulfonyl-N-methyl-6-[(5-methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]pyridine-3-carboxamideKi36.7 [1]
6-[(5-Methyl-3-phenyl-1,2-oxazol-4-yl)methoxy]-N-(1-methylpyrazol-3-yl)pyridine-3-carboxamideKi5.1 [1]
5-(3-Methyl-[1,2,4]oxadiazol-5-yl)-2-(5-methyl-3-phenyl-isoxazol-4-ylmethoxy)-pyridineKi3.3 [1]
2-(5-Methyl-3-phenyl-isoxazol-4-ylmethoxy)-5-(5-methyl-4H-[1,2,4]triazol-3-yl)-pyridineKi1.1 [1]
2-(5-Methyl-3-phenyl-isoxazol-4-ylmethoxy)-5-methylsulfanyl-pyridineKi17.7 [1]
6-[[3-(4-Chlorophenyl)-5-methyl-1,2-oxazol-4-yl]methoxy]-N-[(2R)-1-hydroxypropan-2-yl]pyridine-3-carboxamideKi0.8 [1]
6-[[3-(4-Chlorophenyl)-5-methyl-1,2-oxazol-4-yl]methoxy]-N-[(2S)-1-hydroxypropan-2-yl]pyridine-3-carboxamideKi0.5 [1]
6-[[3-(2,4-Difluorophenyl)-5-methyl-1,2-oxazol-4-yl]methoxy]-N-propan-2-ylpyridine-3-carboxamideKi2.4 [1]
6-[[3-(4-Chlorophenyl)-5-methyl-1,2-oxazol-4-yl]methoxy]-N-[(2S)-1,1,1-trifluoropropan-2-yl]pyridine-3-carboxamideKi1.3 [1]
6-[[3-(2,5-Difluorophenyl)-5-methyl-1,2-oxazol-4-yl]methoxy]-N-propan-2-ylpyridine-3-carboxamideKi27.3 [1]
6-[[3-(2,4-Difluorophenyl)-5-methyl-1,2-oxazol-4-yl]methoxy]-N-(oxan-4-yl)pyridine-3-carboxamideKi2.3 [1]
6-[(5-Methyl-3-pyridin-2-yl-1,2-oxazol-4-yl)methoxy]-N-propan-2-ylpyridine-3-carboxamideKi0.6 [1]
[6-(5-Methyl-3-pyridin-2-yl-isoxazol-4-ylmethoxy)-pyridin-3-yl]-morpholin-4-yl-methanoneKi14.6 [1]
6-[(5-Methyl-3-pyridin-2-yl-1,2-oxazol-4-yl)methoxy]-N-(2,2,2-trifluoroethyl)pyridine-3-carboxamideKi1.1 [1]
[6-(5-Methyl-3-pyridin-2-yl-isoxazol-4-ylmethoxy)-pyridin-3-yl]-thiomorpholin-4-yl-methanoneKi6.8 [1]
6-(5-Methyl-3-pyridin-2-yl-isoxazol-4-ylmethoxy)-nicotinic acidKi22.3 [1]
{6-[3-(5-Fluoro-pyridin-2-yl)-5-methyl-isoxazol-4-ylmethoxy]-pyridin-3-yl}-morpholin-4-yl-methanoneKi4.1 [1]
N-Ethyl-6-[[3-(5-fluoropyridin-2-yl)-5-methyl-1,2-oxazol-4-yl]methoxy]pyridine-3-carboxamideKi0.5 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ GABA receptor alpha-5 subunit Inhibitors (IC50, Ki)." AAT Bioquest, Inc.21 Dec2024https://www.aatbio.com/data-sets/gaba-receptor-alpha-5-subunit-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024December 21). Quest Database™ GABA receptor alpha-5 subunit Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/gaba-receptor-alpha-5-subunit-inhibitors-ic50-ki.
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